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Class 546/279.1 - Nitrogen or -C(=X)-, wherein X is chalcogen, attached directly to the five- membered ring by nonionic bonding


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which nitrogen or -C(=X)-, wherein
No. of patents: 463
Last issue date: 10/25/2011


1                      
NumberTitleIssue Date
8044209Pyrrolydine derivatives as IAP inhibitors
The present invention relates to novel IAP inhibitor compounds of: Formula (I). ...
10/25/2011
7872141Processes for the manufacture of a pyrrolidine-3,4-dicarboxamide derivative
The invention is concerned with processes for the manufacture of the pyrrolidine-3,4-dicarboxamide derivative of formula (I), and the intermediates useful for those processes of manufacture. ...
01/18/2011
7407974Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thro...
08/05/2008
7393865Sleep inducing compounds and methods relating thereto
Compounds having the following structure (I): including stereoisomers, prodrugs, and pharmaceutically acceptable salts, esters and solvates thereof, wherein R1, R2, R3a, R3b, L
07/01/2008
7390907Vanilloid receptor ligands and their use in treatments
Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascu...
06/24/2008
7361663N-acylpyrrolidin-2-ylalkylbenzamidine derivatives as inhibitors of factor Xa
This invention is directed to N-acylpyrrolidin-2-ylalkylbenzamidine derivatives which useful for inhibiting the activity of Factor Xa, by contacting said derivatives with a composition containing Factor Xa. The present invention is also directed to compositions cont...
04/22/2008
7354939Pyrrole inhibitors of ERK protein kinase, synthesis thereof and intermediates thereto
The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, ...
04/08/2008
7297693Nitrogen-containing heterocyclic compounds and their use as Raf inhibitors
Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy. ...
11/20/2007
7279470Compounds and uses thereof for decreasing activity of hormone-sensitive lipase
Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may...
10/09/2007
72591634-(6-membered)-heteroaryl acyl pyrrolidine derivatives as HCV inhibitors
Novel anti-viral agents of Formula wherein: A represents OR1, NR1R2, or R1 wherein R1 and R2 are hydrogen, C1-6alkyl, aryl...
08/21/2007
7253187Heterocyclic inhibitors of ERK2 and uses thereof
Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein Z1 and Z2 are each independently nitrogen or CH and Ring A, TmR1...
08/07/2007
7250443Pyrrole based inhibitors of glycogen synthase kinase 3
New pyrrole based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed al...
07/31/2007
7241745Pyridyl alkene and pyridyl alkine acid amides as cytostatics and immunosupressives
The invention relates to a new pyridyl alkene and pyridyl alkine acid amides according to the general formula (I) as well as methods for their production, medicaments containing these compounds as well as their m...
07/10/2007
7238683Fused phenylalanine derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
The present invention is directed to fused phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-RV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is in...
07/03/2007
7230017Dihydropyridinone derivatives
The invention relates to novel dihydropyridinone derivatives, processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failur...
06/12/2007
7230002Dipeptidyl peptidase IV inhibitors; processes for their preparation and compositions thereof
The present invention relates to novel dipeptidyl peptidase IV (DPP-IV) inhibitors their analogs, isomers, pharmaceutical compositions, therapeutic uses and methods of making the same. ...
06/12/2007
7223788Substituted N-aryl heterocycles, process for their preparation and their use as medicaments
The invention relates to substituted N-aryl heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof. Compounds of the formula I in which the radicals have...
05/29/2007
7186735Acylated arylcycloalkylamines and their use as pharmaceuticals
The present invention relates to acylated arylcycloalkylamines, to pharmaceutical compositions comprising such compounds, to methods for the stimulation of the expression of endothelial NO synthase, and methods of treatment comprising administering such compounds.
03/06/2007
7186843Aminomethylpyrrolidine derivatives having aromatic substituents
This invention provides a quinolone derivative having potent antibacterial activity against various bacteria including drug-resistant strains which is a compound of the following formula wherein R1 is an optionally substituted aromatic group, a salt of th...
03/06/2007
7183290Fluoropyrrolidines as dipeptidyl peptidase inhibitors
The present invention relates to novel compounds, their use for inhibiting post prolin/analine-cleaving proteases, such as serine proteases, such as dipeptidyl peptidases, such as dipeptidyl peptidase IV (DPP-IV), and to methods for their production and their therap...
02/27/2007
7148242N-formyl hydroxylamine compounds, compositions and methods of use
N-[1-oxo-2-alkyl-3-(N-hydroxyformamido)-propyl]-(carbonylamino-aryl or -heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes or imidazacyclo4-7alkanes have interesting properties, e.g., in the treatment or prevention of disorders ...
12/12/2006
7144886Dipeptidyl peptidase IV (DP-IV) inhibitors as anti-diabetic agents
The present invention relates to a series of prodrugs of inhibitors of DP-IV with improved properties. The compounds can be used for the treatment of a number of human diseases, including impaired glucose tolerance and type II diabetes. The compounds of the inventio...
12/05/2006
71354723-Heterocyclic benzylamide derivatives as potassium channel openers
The present invention provides novel 3-heterocyclic benzylamides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6
11/14/2006
7132543Para-phenylenediamine derivatives containing a disubstituted pyrrolidinyl group bearing a cationic radical, and use of the same for dyeing keratin fibers
The present disclosure relates to a novel a para-phenylenediamine derivative substituted with a pyrrolidinyl group of formula (I) and the addition salts thereof. The present disclosure also relates to a dyeing composition for keratin fibers comprising the paraphenyl...
11/07/2006
7126007Process for preparing pyrrolidinyl-functional para-phenylenediamine derivatives substituted by a nitrogenous radical, and intermediate compounds
A process for synthesizing para-phenylenediamine derivative compounds containing a pyrolidinyl group, and substituted by a nitrogenous radical, wherein the para-phenylenediamine derivative compounds are chosen from those of formula (I):
10/24/2006
7125863Inhibitors of dipeptidyl peptidase IV
Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of t...
10/24/2006
7109150Trifluoromethylpyrrolecarboxamides and trifluoromethylpyrrolethioamides as fungicides
Novel pyrrole derivatives of formula I wherein X is oxygen or sulfur; R1 is hydrogen, C1–C4alkyl unsubstituted or substituted, or halogen;
09/19/2006
7105556Conformationally constrained analogs useful as antidiabetic and antiobesity agents and method
Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2
09/12/2006
7105546Acyclic and cyclic amine derivatives
The present invention relates to acyclic and cyclic amine derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizin...
09/12/2006
7105513Acylated, heteroaryl-condensed cycloalkenylamines and their use as pharmaceuticals
The present invention relates to acylated, heteroaryl-condensed cycloalkenylamines, to pharmaceutical compositions comprising such compounds, to methods for the stimulation of the expression of endothelial NO synthase, and methods of treatment comprising administeri...
09/12/2006
7087628N-heterocyclyl hydrazides as neurotrophic agents
This invention relates to a series of N-heterocyclyl hydrazides of Formula I, and pharmaceutical compositions containing them. The compounds of the invention have neurotrophic activity and are useful in the treat...
08/08/2006
RE39140Heterocyclic compounds
Novel heterocyclic compounds of the formula wherein, R1 represents a hydrogen atom or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by...
06/20/2006
RE39130Heterocyclic compounds
Novel heterocyclic compounds of the formula wherein, R1 represents a hydrogen atom or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by...
06/13/2006
RE39129Heterocyclic compounds
Novel heterocyclic compounds of the formula wherein, R1 represents a hydrogen atom or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by...
06/13/2006
RE39127Heterocyclic compounds
Novel heterocyclic compounds of the formula wherein, R1 represents a hydrogen atom or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by...
06/13/2006
RE39131Heterocyclic compounds
Novel heterocyclic compounds of the formula wherein, R1 represents a hydrogen atoms or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted b...
06/13/2006
7030141Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat...
04/18/2006
7005437Substituted aryl and heteroaryl derivatives, the preparation thereof and the use therof as pharmaceutical compositions
The present invention relates to new substituted aryl and heteroaryl derivatives of general formula wherein A, Ar, n, X, Y1, Y2, Y3, Y4, R
02/28/2006
6995174Hepatitis C virus inhibitors
Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R′, B, Y and X are described in the description. Composit...
02/07/2006
6949539Admantane derivatives
The invention provides compounds of general formula (I) in which m, A, R1 and Ar have the meanings defined in the specification; a process for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compo...
09/27/2005
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